2-[1-(2-tert-butyl-6-chloro-5-methyl-pyrimidin-4-yl)-piperidin-4-yl]-[1,8]naphthyridine | 870089-68-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 2-[1-(2-tert-butyl-6-chloro-5-methyl-pyrimidin-4-yl)-piperidin-4-yl]-[1,8]naphthyridine
• 英文别名: 2-[1-(2-Tert-butyl-6-chloro-5-methyl-pyrimidin-4-yl)-piperidin-4-yl]-[1,8]naphthyridine；2-[1-(2-tert-butyl-6-chloro-5-methylpyrimidin-4-yl)piperidin-4-yl]-1,8-naphthyridine
• CAS: 870089-68-2
• 化学式: C₂₂H₂₆ClN₅
• 分子量: 395.935
• InChiKey: ZOVCDQRVJZPZMO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  54.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-[1-(2-tert-butyl-6-chloro-5-methyl-pyrimidin-4-yl)-piperidin-4-yl]-[1,8]naphthyridine 在 platinum(IV) oxide 、 tris-(dibenzylideneacetone)dipalladium(0) 氢气 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 cesium fluoride 作用下， 以 1,4-二氧六环 、 乙醇 为溶剂， 反应 21.0h， 生成 tert-butyl 2-benzyloxycarbonylamino-3-[2-tert-butyl-5-methyl-6-[4-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-piperidin-1-yl]-pyrimidin-4-ylamino]-propionate
  参考文献：
  名称：

  Pyrimidine Derivatives Which Are Antagonists Of Vitronectin Receptor

  摘要：

  本发明的主题是公式(I)的化合物；其中R1、R2、R3、R4和R具有说明书中指出的含义，它们的制备过程，它们作为对玻连蛋白受体具有拮抗活性的药物的使用以及包含它们的药物组合物。

  公开号：

  US20080058348A1
• 作为产物：
  描述：

  2,2-二甲基丙亚胺盐酸 在 sodium ethanolate 、 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 乙醇 、 异丁酰胺 为溶剂， 反应 7.5h， 生成 2-[1-(2-tert-butyl-6-chloro-5-methyl-pyrimidin-4-yl)-piperidin-4-yl]-[1,8]naphthyridine
  参考文献：
  名称：

  Pyrimidine Derivatives Which Are Antagonists Of Vitronectin Receptor

  摘要：

  本发明的主题是公式(I)的化合物；其中R1、R2、R3、R4和R具有说明书中指出的含义，它们的制备过程，它们作为对玻连蛋白受体具有拮抗活性的药物的使用以及包含它们的药物组合物。

  公开号：

  US20080058348A1

文献信息

• METHODS FOR THE USE OF PYRIMIDINE DERIVATIVES WHICH ARE ANTAGONISTS OF VITRONECTIN RECEPTOR
  申请人：Lefrancois Jean-Michel

  公开号：US20100041675A1

  公开（公告）日：2010-02-18

  A subject of the invention is the compounds of formula (I); in which R 1 , R 2 , R 3 , R 4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.

  本发明的主题是式(I)的化合物;其中R1、R2、R3、R4和R的含义如说明书中所示，它们的制备过程，它们作为具有抗vitronectin受体活性的药物的用途以及包含它们的制药组合物。
• Methods for the use of pyrimidine derivatives which are antagonists of vitronectin receptor
  申请人：Galapagos SAS

  公开号：US07846932B2

  公开（公告）日：2010-12-07

  A subject of the invention is the compounds of formula (I); in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.

  该发明的主题是公式（I）的化合物；其中R1、R2、R3、R4和R具有说明书中所示的含义，它们的制备过程，它们作为具有对vitronectin受体拮抗活性的药物的用途以及包含它们的制药组合物。
• Pyrimidine derivatives which are antagonists of vitronectin receptor
  申请人：Galapagos SAS

  公开号：US07825119B2

  公开（公告）日：2010-11-02

  A subject of the invention is the compounds of formula (I): in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.

  本发明的主题是公式（I）的化合物：其中R1，R2，R3，R4和R具有说明书中指示的含义，它们的制备过程，它们作为具有抗维糖蛋白受体活性的药物的用途以及含有它们的制药组合物。
• PYRIMIDINE DERIVATIVES WHICH ARE ANTAGONISTS OF THE VITRONECTIN RECEPTOR
  申请人：Lefrancois Jean-Michel

  公开号：US20120115883A1

  公开（公告）日：2012-05-10

  A subject of the invention is the compounds of formula (I); in which R 1 , R 2 , R 3 , R 4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.

  本发明的主题是式(I)的化合物；其中R1、R2、R3、R4和R具有说明中所示的含义，它们的制备过程，它们作为拥有对vitronectin受体拮抗活性的药物的用途以及含有它们的制药组合物。
• Pyrimidine derivatives which are antagonist of the vitronectin receptor
  申请人：Galapagos NV

  公开号：US08133896B2

  公开（公告）日：2012-03-13

  A subject of the invention is the compounds of formula (I); in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.

  本发明的主题是公式(I)化合物；其中R1、R2、R3、R4和R具有说明中所示的含义，它们的制备过程，它们作为具有抗血浆粘附素受体活性的药物的用途以及包含它们的制药组合物。